BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC 50 of 2.5 nM in the adhesion assay and an IC 50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model.
性状
Solid
体外研究(In Vitro)
BMS-688521 in a mouse specific adhesion assay employed mouse splenocytes and a mouse ICAM-1 expression cell line, b.END3. BMS-688521 has an IC50 of 78 nM, representing an approximately 30-fold decrease in activity relative to the human T-cell/HUVEC assay data (ICIC50=2.5 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
BMS-688521 (1-10 mg/kg; p.o.; BID for a three-day) is efficacious in a mouse allergic eosinophilic lung inflammation model.
BMS-688521 (5 mg/kg; p.o.) treatment shows the C max , T max , AUC, F values are 0.32 μM, 1.0 μM, 1.5 μM h, and 50%, respectively.
BMS-688521 (1 mg/kg; i.v.) treatment shows the T 1/2 , MRT, CL and Vss values are 1.6 hours, 1.7 hours, 50 mL/mim/kg, and 5.1 L/kg, respectively in BALB/c mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Watterson SH, et al. Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4
溶解度数据
In Vitro: DMSO : 100 mg/mL (186.44 mM; Need ultrasonic)配制储备液